C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 255/47 (2006.01) A61K 31/26 (2006.01) C07F 7/08 (2006.01)
Patent
CA 2670099
This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE- 31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-.gamma., induce heme oxygenase-1 (HO-1), induce CD11b expression - a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
La présente invention concerne de nouveaux dérivés tricycliques-bis-énones (TBE), tels que TBE-31, TBE-34, TBE-45 et TBE hydrosolubles. Les procédés de préparation de ces composés sont également proposés. Les inventeurs démontrent la capacité de ces nouveaux composés TBE à inhiber la prolifération de cellules de myélome humain, inhiber l'induction de l'iNOS dans les cellules stimulées par l'interféron-.gamma., induire l'hémo-oxygénase-1 (HO-1), induire l'expression de CD1 1b - un marqueur différentiel de la leucémie, inhiber la prolifération des cellules leucémiques, induire l'apoptose dans le cancer du poumon humain et induire l'apoptose dans d'autres cellules cancéreuses. Les TBE de la présente invention sont censées être des agents utiles pour le traitement et la prévention de nombreuses maladies comprenant le cancer, les troubles neurologiques, l'inflammation et les pathologies liées au stress oxydatif.
Gribble Gordon W.
Honda Tadashi
Sporn Michael B.
Sundararajan Chitra
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Trustees Of Dartmouth College
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